The hybrid approach, encompassing two pharmacophores in one molecular scaffold, has attracted much attention in medicinal chemistry. In this study, we synthesized a panel of hybrid molecules based on the natural active ingredients, β-ionone and 3,4,5-trimethoxycinnamic acid. The results exhibited that 3,4,5-trimethoxy-hybrid displayed the most excellent cytotoxicity against cancer cells, whereas, the electron effect of substituents plays no distinct effect on antiproliferative activity. The cytotoxicity of 3,4,5-trimethoxy-hybrid may be due to its cell cycle arrest and apoptosis-inducing activities, which may be relationship with the reactive oxygen species generation, redox imbalance, lipid peroxidation and the collapse of mitochondrial membrane potential induced by 3,4,5-trimethoxy-hybrid in A549 (human lung adenocarcinoma) cells. In conclusion, 3,4,5-trimethoxy-hybrid could induce cancer cell apoptosis through the reactive oxygen species generation.

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中文翻译：

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肉桂酸/β-紫罗兰酮杂化物：合成和体外抗癌活性评价

在一个分子支架中包含两个药效团的混合方法在药物化学中引起了很多关注。在这项研究中，我们合成了一组基于天然活性成分 β-紫罗兰酮和 3,4,5-三甲氧基肉桂酸的杂化分子。结果表明，3,4,5-三甲氧基杂化物对癌细胞显示出最优异的细胞毒性，而取代基的电子效应对抗增殖活性没有明显影响。3,4,5-三甲氧基杂化物的细胞毒性可能是由于其细胞周期阻滞和凋亡诱导活性，这可能与活性氧的产生、氧化还原失衡、脂质过氧化和线粒体膜电位的崩溃有关。通过 A549（人肺腺癌）细胞中的 3,4,5-三甲氧基杂化物。综上所述，

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